WO2003051366A3 - Inhibiteurs de kinase - Google Patents

Inhibiteurs de kinase Download PDF

Info

Publication number
WO2003051366A3
WO2003051366A3 PCT/US2002/039915 US0239915W WO03051366A3 WO 2003051366 A3 WO2003051366 A3 WO 2003051366A3 US 0239915 W US0239915 W US 0239915W WO 03051366 A3 WO03051366 A3 WO 03051366A3
Authority
WO
WIPO (PCT)
Prior art keywords
phenyl
cancer
treatment
alkoxy
kinase inhibitors
Prior art date
Application number
PCT/US2002/039915
Other languages
English (en)
Other versions
WO2003051366A2 (fr
Inventor
Qun Li
Keith W Woods
Gui-Dong Zhu
John P Fischer
Jianchun Gong
Tongmei Li
Viraj Gandhi
Sheela A Thomas
Garrick Packard
Xiaohong Song
Jason N Abrams
Robert Diebold
Jurgen Dinges
Charles Hutchins
Vincent S Stoll
Saul H Rosenberg
Vincent L Giranda
Original Assignee
Abbott Lab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Abbott Lab filed Critical Abbott Lab
Priority to AU2002353147A priority Critical patent/AU2002353147A1/en
Priority to JP2003552299A priority patent/JP2005516927A/ja
Priority to CA002470214A priority patent/CA2470214A1/fr
Priority to EP02790126A priority patent/EP1463505A2/fr
Publication of WO2003051366A2 publication Critical patent/WO2003051366A2/fr
Publication of WO2003051366A3 publication Critical patent/WO2003051366A3/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/02Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4

Abstract

L'invention porte sur des composés représentés par la formule (I), utiles dans l'inhibition de protéines kinases. L'invention concerne aussi des compositions qui inhibent des protéines kinases et des procédés d'inhibition des protéines kinases chez un patient.
PCT/US2002/039915 2001-12-13 2002-12-12 Inhibiteurs de kinase WO2003051366A2 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU2002353147A AU2002353147A1 (en) 2001-12-13 2002-12-12 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancer
JP2003552299A JP2005516927A (ja) 2001-12-13 2002-12-12 癌治療用のキナーゼ阻害剤としての3−(フェニル−アルコキシ)−5−(フェニル)−ピリジン誘導体および関連化合物
CA002470214A CA2470214A1 (fr) 2001-12-13 2002-12-12 Inhibiteurs de kinase
EP02790126A EP1463505A2 (fr) 2001-12-13 2002-12-12 Derives de la 3-(phenyl-alkoxy)-5-(phenyl)-pyridine et composes similaires avec activite inhibiteur de kinase pour le traitement du cancer.

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US2336301A 2001-12-13 2001-12-13
US34135601P 2001-12-13 2001-12-13
US10/023,363 2001-12-13
US34147401P 2001-12-17 2001-12-17
US10/295,833 2002-11-18
US10/295,833 US20030187026A1 (en) 2001-12-13 2002-11-18 Kinase inhibitors
US10/317,914 US6831175B2 (en) 2001-12-13 2002-12-12 Kinase inhibitors

Publications (2)

Publication Number Publication Date
WO2003051366A2 WO2003051366A2 (fr) 2003-06-26
WO2003051366A3 true WO2003051366A3 (fr) 2004-03-25

Family

ID=29554492

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/039915 WO2003051366A2 (fr) 2001-12-13 2002-12-12 Inhibiteurs de kinase

Country Status (2)

Country Link
US (2) US20030187026A1 (fr)
WO (1) WO2003051366A2 (fr)

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8846714B2 (en) 2009-12-21 2014-09-30 Samumed, Llc 1H-pyrazolo[3,4-β]pyridines and therapeutic uses thereof
US8883822B2 (en) 2012-05-04 2014-11-11 Samumed, Llc 1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
US8987298B2 (en) 2012-04-04 2015-03-24 Samumed, Llc Indazole inhibitors of the Wnt signal pathway and therapeutic uses thereof
US9221793B2 (en) 2011-09-14 2015-12-29 Samumed, Llc Indazole-3-carboxamides and their use as Wnt/β-catenin signaling pathway inhibitors
US9365548B2 (en) 2006-03-31 2016-06-14 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor
US9381192B2 (en) 2009-08-10 2016-07-05 Samumed, Llc Indazole inhibitors of the Wnt signal pathway and therapeutic uses thereof
US9394285B2 (en) 2013-03-15 2016-07-19 Pfizer Inc. Indole and indazole compounds that activate AMPK
US9447071B2 (en) 2014-02-07 2016-09-20 Global Blood Therapeutics, Inc. Crystalline polymorphs of the free base of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
US9475825B2 (en) 2014-09-08 2016-10-25 Samumed, Llc 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridine and therapeutic uses thereof
US9475807B2 (en) 2014-09-08 2016-10-25 Samumed, Llc 2-(1H-indazol-3-yl)-1H-imidazo[4,5-C]pyridine and therapeutic uses thereof
US9493487B2 (en) 2014-09-08 2016-11-15 Samumed, Llc 3-(1H-imidazo[4,5-C]pyridin-2-YL)-1H-pyrazolo[3,4-B]pyridine and therapeutic uses thereof
US9540398B2 (en) 2014-09-08 2017-01-10 Samumed, Llc 3-(1h-imidazo[4,5-C]pyridin-2-yl)-1h-pyrazolo[3,4-C]pyridine and therapeutic uses thereof
US9546185B2 (en) 2014-09-08 2017-01-17 Samumed, Llc 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridine and therapeutic uses thereof

Families Citing this family (228)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002252614B2 (en) 2001-04-10 2006-09-14 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
JP4394960B2 (ja) 2002-04-08 2010-01-06 メルク エンド カムパニー インコーポレーテッド Akt活性阻害薬
EP1541559A4 (fr) * 2002-07-22 2007-08-22 Asahi Kasei Pharma Corp Derive d'isoquinoline 5-substituee
CA2495216A1 (fr) * 2002-08-12 2004-02-19 Sugen, Inc. 3-pyrrolyl-pyridopyrazoles et 3-pyrrolyl-indazoles utilises en tant que nouveaux inhibiteurs de la proteine kinase
US20050282814A1 (en) * 2002-10-03 2005-12-22 Targegen, Inc. Vasculostatic agents and methods of use thereof
GB2400101A (en) * 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
US7297709B2 (en) 2003-05-22 2007-11-20 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
US7129260B2 (en) 2003-06-02 2006-10-31 Abbott Laboratories Isoindolinone kinase inhibitors
EP1633710A1 (fr) * 2003-06-02 2006-03-15 Abbott Laboratories Composes d'isoindoline-1-one utilises en tant qu'inhibiteurs de kinase
US7531529B2 (en) * 2003-06-05 2009-05-12 Roche Palo Alto Llc Imidazole derivatives
WO2005003101A2 (fr) * 2003-07-02 2005-01-13 Biofocus Discovery Limited Composes se liant au site actif d'enzymes proteine kinases
US6984652B2 (en) * 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
WO2005027907A1 (fr) * 2003-09-17 2005-03-31 Icos Corporation Utilisation d'inhibiteurs de la chk1 pour lutter contre la proliferation cellulaire
TW200526631A (en) * 2003-10-07 2005-08-16 Renovis Inc Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
US7781591B2 (en) * 2006-06-13 2010-08-24 Wyeth Llc Substituted 3-cyanopyridines as protein kinase inhibitors
JP4768628B2 (ja) * 2003-11-19 2011-09-07 アレイ バイオファーマ、インコーポレイテッド Mekの二環系阻害剤及びその使用方法
AU2004293026B2 (en) * 2003-11-21 2012-01-19 Array Biopharma Inc. AKT protein kinase inhibitors
US20050137204A1 (en) * 2003-12-22 2005-06-23 Abbott Laboratories Fused bicycloheterocycle substituted quinuclidine derivatives
US20070060588A1 (en) * 2003-12-22 2007-03-15 Jianguo Ji Fused bicycloheterocycle substituted quinuclidine derivatives
US7655657B2 (en) * 2003-12-22 2010-02-02 Abbott Laboratories Fused bicycloheterocycle substituted quinuclidine derivatives
US7160876B2 (en) 2003-12-22 2007-01-09 Abbott Laboratories Fused bicycloheterocycle substituted quinuclidine derivatives
US20050245531A1 (en) * 2003-12-22 2005-11-03 Abbott Laboratories Fused bicycloheterocycle substituted quinuclidine derivatives
US20070185152A1 (en) * 2004-03-02 2007-08-09 Smithkline Beecham Corporation Inhibitors of akt activity
EP2543376A1 (fr) * 2004-04-08 2013-01-09 Targegen, Inc. Inhibiteurs de benzotriazine de kinases
GEP20084550B (en) * 2004-04-30 2008-11-25 Warner Lambert Co Substituted morpholine compounds for the treatment of central nervous system disorders
GB0409744D0 (en) * 2004-04-30 2004-06-09 Pfizer Ltd Novel compounds
US20060074102A1 (en) * 2004-05-14 2006-04-06 Kevin Cusack Kinase inhibitors as therapeutic agents
BRPI0511678A (pt) 2004-06-01 2008-01-08 Hoffmann La Roche piridin-4-il-etinil-imidazóis e pirazóis como antagonistas de receptor de mglu5
FR2871158A1 (fr) * 2004-06-04 2005-12-09 Aventis Pharma Sa Indazoles substitues, compositions les contenant, procede de fabrication et utilisation
WO2006000589A1 (fr) * 2004-06-28 2006-01-05 Altana Pharma Ag Pyrimidines 4,6-disubstituees et leur utilisation comme inhibiteurs des proteines kinases
KR20070043996A (ko) * 2004-07-02 2007-04-26 이코스 코포레이션 Chk1의 억제에 유용한 화합물
US7626021B2 (en) * 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
AU2005269387A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
CA2576172A1 (fr) * 2004-08-23 2006-04-06 Merck & Co., Inc. Inhibiteurs de l'activite de akt
JP5275628B2 (ja) 2004-08-25 2013-08-28 ターゲジェン インコーポレーティッド 複素環式化合物および使用方法
AU2005286592A1 (en) * 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
JP4954086B2 (ja) * 2004-12-08 2012-06-13 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 1h−ピロロ[2,3−b]ピリジン
US7576099B2 (en) * 2005-02-28 2009-08-18 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
BRPI0606365A2 (pt) * 2005-02-28 2017-06-27 Renovis Inc composto ou um sal, solvato ou pró-droga farmaceuticamente aceitável do mesmo e estereoisômeros e tautômeros do mesmo, composição farmacêutica, métodos para prevenir, tratar, melhorar ou controlar uma doença ou condição e para preparar um composto, uso de um composto ou um sal, solvato ou composição farmaceuticamente aceitável do mesmo, método de tratamento de um mamífero, e, combinação
WO2006094034A1 (fr) * 2005-03-01 2006-09-08 Wyeth Composes de cinnoline et leur utilisation comme modulateurs du recepteur hepatique x
WO2006101977A2 (fr) * 2005-03-16 2006-09-28 Targegen, Inc. Composes de pyrimidine et methodes d'utilisation
US8093244B2 (en) 2005-03-29 2012-01-10 Icos Corporation Heteroaryl urea derivatives useful for inhibiting CHK1
US20060264439A1 (en) * 2005-05-17 2006-11-23 Supergen, Inc. Inhibitors of polo-like kinase-1
SG177981A1 (en) * 2005-05-18 2012-02-28 Array Biopharma Inc 4-(phenylamino)-6-oxo-1, 6-dihydropyridazine-3-carboxamide derivatives as mek inhibitors for the treatment of hyperproliferative diseases
MX2007008848A (es) * 2005-06-08 2008-04-16 Targegen Inc Metodos y composiciones para el tratamiento de desordenes oculares.
EP1898903B8 (fr) 2005-06-10 2013-05-15 Merck Sharp & Dohme Corp. Inhibiteurs de l'activite akt
SI1898903T1 (sl) * 2005-06-10 2013-07-31 Merck Sharp & Dohme Corp. Inhibitorji akt aktivnosti
EP2719384B1 (fr) 2005-07-27 2018-08-08 Otsuka America Pharmaceutical, Inc. Nouvelle préparation de 1-naphthyl-3-azabicyclo[3.1.0]hexanes et utilisation pour le traitement de troubles neurophychiatriques
CA2620631A1 (fr) 2005-08-29 2007-03-08 Vertex Pharmaceuticals Incorporated Utilisation de pyridones en tant qu'inhibiteurs de kinases
EP1919906B1 (fr) 2005-08-29 2011-10-12 Vertex Pharmaceuticals Incorporated Pyrid-2-ones disubstituees en 3, 5 inhibitrices de la famille tec des tyrosine kinases non receptrices
ATE548363T1 (de) * 2005-08-29 2012-03-15 Vertex Pharma 3,5-disubstituierte pyrid-2-one, die sich als inhibitoren der tec-familie von nicht-rezeptor- tyrosinkinasen eignen
CA2628283C (fr) * 2005-11-01 2017-06-27 Targegen, Inc. Inhibiteurs de kinase de type biaryl-meta-pyrimidine
US8604042B2 (en) * 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) * 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US20070149508A1 (en) * 2005-11-02 2007-06-28 Targegen, Inc. Six membered heteroaromatic inhibitors targeting resistant kinase mutations
NL2000284C2 (nl) 2005-11-04 2007-09-28 Pfizer Ltd Pyrazine-derivaten.
PL1954699T3 (pl) * 2005-11-22 2013-01-31 Kudos Pharm Ltd Pochodne pirydo-, pirazo- i pirymidopirymidyny jako inhibitory mTOR
US8546404B2 (en) * 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
EP1971611B1 (fr) 2005-12-21 2012-10-10 Abbott Laboratories Composes anti-viraux
RU2441869C2 (ru) * 2005-12-21 2012-02-10 Эбботт Лэборетриз Противовирусные соединения
MX2008008328A (es) 2005-12-22 2008-09-15 Alcon Res Ltd (indazol-5-il)-pirazinas y (1,3-dihidro-indol-2-ona)-pirazinas para tratar enfermedades y condiciones mediadas con rho cinasa.
PL1993360T3 (pl) 2005-12-28 2017-08-31 Vertex Pharmaceuticals Incorporated Stałe postacie n-[2,4-bis(1,1-dimetyloetylo)-5-hydroksyfenylo]-1,4- dihydro-4-oksochinolino-3-karboksyamidu
CA2635580A1 (fr) * 2005-12-30 2007-07-12 Alantos Pharmaceuticals Holding, Inc. Inhibiteurs de metalloproteases a base de bisamides substitues
WO2007097937A1 (fr) * 2006-02-16 2007-08-30 Schering Corporation Nouveaux composés inhibiteurs erk
WO2007106884A2 (fr) 2006-03-15 2007-09-20 Theralogics, Inc. Méthodes de traitement des maladies d'atrophie musculaire au moyen d'inhibiteurs de l'activation de nf-kb
EP2001870A2 (fr) * 2006-03-31 2008-12-17 Schering Corporation Inhibiteurs de kinase
PL2018380T3 (pl) 2006-05-19 2012-05-31 Abbvie Bahamas Ltd Skondensowane azabicykliczne pochodne alkanowe podstawione bicykloheterocyklem o aktywności wobec OUN
WO2007135398A1 (fr) * 2006-05-22 2007-11-29 Astrazeneca Ab Dérivés de l'indole
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
UA99597C2 (ru) * 2006-07-06 2012-09-10 Еррей Біофарма Інк. Пиримидилциклопентаны как ингибиторы акт протеинкиназ
DE602007011628D1 (de) 2006-07-06 2011-02-10 Array Biopharma Inc Dihydrofuropyrimidine als akt-proteinkinaseinhibitoren
WO2008006039A1 (fr) 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrothiéno pyrimidines comme inhibiteurs de la protéine kinase akt
LT2057156T (lt) 2006-08-23 2017-05-25 Kudos Pharmaceuticals Limited 2-metilmorfolino pirido-, pirazo- ir pirimidopirimidino dariniai kaip mtor slopikliai
US7678803B2 (en) * 2006-08-24 2010-03-16 Serenex, Inc. Quinazoline derivatives for the treatment of cancer
US7776589B1 (en) 2006-08-31 2010-08-17 Schering Corporation Polynucleotides encoding polypeptide fragments of protein kinase B gamma (AKT3)
GB0619325D0 (en) * 2006-09-30 2006-11-08 Univ Strathclyde New compounds
ES2633318T3 (es) 2006-10-23 2017-09-20 Cephalon, Inc. Derivados bicíclicos fusionados de 2,4-diaminopirimidina como inhibidores de ALK y c-Met
US7674091B2 (en) * 2006-11-14 2010-03-09 The Boeing Company Rotor blade pitch control
EP2086644A2 (fr) * 2006-11-17 2009-08-12 Schering Corporation Combinaison d'un inhibiteur de l'adn polymerase-alpha avec un inhibiteur d'une kinase de point de controle pour le traitement des maladies proliferatives
AR064010A1 (es) * 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
WO2008070134A1 (fr) * 2006-12-06 2008-06-12 Merck & Co., Inc. Inhibiteurs de l'activité akt
US20100022517A1 (en) * 2006-12-18 2010-01-28 Richards Lori A Ophthalmic formulation of rho kinase inhibitor compound
US8071779B2 (en) * 2006-12-18 2011-12-06 Inspire Pharmaceuticals, Inc. Cytoskeletal active rho kinase inhibitor compounds, composition and use
US8236950B2 (en) 2006-12-20 2012-08-07 Abbott Laboratories Anti-viral compounds
WO2008082840A1 (fr) * 2006-12-29 2008-07-10 Abbott Laboratories Inhibiteurs de la pim kinase utilisés comme agents chimiothérapeutiques contre le cancer
JP2010518014A (ja) * 2007-01-31 2010-05-27 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用な2−アミノピリジン誘導体
CA2679198C (fr) 2007-02-26 2011-07-12 Pfizer Products Inc. Composes heterocycliques utiles dans le traitement de maladies et de conditions
BRPI0810202A2 (pt) 2007-05-03 2014-10-21 Pfizer Ltd Derivados de piridina
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
CA2692502C (fr) 2007-07-05 2016-03-01 Array Biopharma Inc. Cyclopentanes de pyrimidyle comme inhibiteurs de proteines kinases akt
EP2173723B3 (fr) * 2007-07-05 2014-11-19 Array Biopharma Inc. Pyrimidyl cyclopentanes utilsés comme inhibiteurs de la protéine kinase akt
WO2009038784A1 (fr) * 2007-09-21 2009-03-26 Amgen Inc. Composés hétéroaryliques fusionnés de triazole en tant qu'inhibiteurs de kinase p38
AU2008331733A1 (en) 2007-11-02 2009-06-11 Vertex Pharmaceuticals Incorporated [1H- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase C-theta
WO2009067586A1 (fr) 2007-11-21 2009-05-28 Abbott Laboratories Dérivés de diazabicycloalcane à substitution biaryle
KR101624752B1 (ko) * 2008-01-09 2016-05-26 어레이 바이오파마 인크. Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄
WO2009089459A1 (fr) * 2008-01-09 2009-07-16 Array Biopharma Inc. Pyrimidylcyclopentanes hydroxylés utilisés comme inhibiteurs de protéine kinase akt
CA2714743C (fr) * 2008-02-19 2017-01-17 Janssen Pharmaceutica N.V. Aryl-hydroxyethylamino-pyrimidines et triazines en tant que modulateurs d'amide d'acide gras hydrolase
CN102015693B (zh) * 2008-02-21 2014-10-29 默沙东公司 作为erk抑制剂的化合物
CN102066339B (zh) 2008-04-16 2014-09-24 波托拉医药品公司 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物
ES2398423T3 (es) * 2008-06-20 2013-03-19 Astrazeneca Ab Composiciones con y procedimiento para pirido[2,3-D]pirimidinas sustituídas con metilmorfolina
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
MX2011000839A (es) 2008-07-23 2011-04-05 Vertex Pharma Inhibidores de pirazolpiridina cinasa.
US8569337B2 (en) 2008-07-23 2013-10-29 Vertex Pharmaceuticals Incorporated Tri-cyclic pyrazolopyridine kinase inhibitors
WO2010011768A1 (fr) 2008-07-23 2010-01-28 Vertex Pharmaceuticals Incorporated Inhibiteurs de pyrazolopyridine kinase tricylique
WO2010017350A1 (fr) 2008-08-06 2010-02-11 Vertex Pharmaceuticals Incorporated Inhibiteurs d’aminopyridine kinase
US8299055B2 (en) 2008-10-02 2012-10-30 Asahi Kasei Pharma Corporation 8-substituted isoquinoline derivative and the use thereof
EP2379561B1 (fr) 2008-11-25 2015-11-04 University Of Rochester Inhibiteurs de mlk et procédés d'utilisation
RU2016141566A (ru) 2008-12-19 2018-12-20 Вертекс Фармасьютикалз Инкорпорейтед Производные пиразина, используемые в качестве ингибиторов киназы atr
UY32582A (es) * 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
EP2427464A1 (fr) 2009-05-06 2012-03-14 Vertex Pharmaceuticals Incorporated Pyrazolopyridines
US8778972B2 (en) 2009-05-15 2014-07-15 Novartis Ag 5-pyridin-3-yl-1, 3-dihydro-indol-2-on derivatives and their use as modulators of aldosterone synthase and/or CYP11B1
CA2761853A1 (fr) 2009-05-15 2010-11-18 Novartis Ag Derives de benzoxazolone en tant qu'inhibiteurs d'aldosterone synthase
ES2459468T3 (es) 2009-05-15 2014-05-09 Novartis Ag Arilpiridinas como inhibidores de aldosterona sintasa
WO2011019648A1 (fr) * 2009-08-10 2011-02-17 Epitherix, Llc Indazoles utiles comme inhibiteurs de la voie de signalisation de wnt/bêta-caténine et utilisations thérapeutiques de ceux-ci
US8906914B2 (en) 2009-08-18 2014-12-09 Janssen Pharmaceutica Nv Ethylene diamine modulators of fatty acid hydrolase
US8513271B2 (en) 2009-10-30 2013-08-20 Janssen Pharmaceutica, Nv Pyrimidine compounds as delta opioid receptor modulators
JP5770198B2 (ja) 2009-10-30 2015-08-26 ヤンセン ファーマシューティカ エヌ.ベー. オピオイド受容体調節因子としてのフェノキシ置換ピリミジン
AU2010313392B2 (en) 2009-10-30 2015-07-09 Janssen Pharmaceutica Nv Pyrazines as delta opioid receptor modulators
CN102762560A (zh) 2009-12-21 2012-10-31 诺瓦提斯公司 二取代的杂芳基-稠合的吡啶
CA2787321A1 (fr) * 2010-01-27 2011-08-04 Vertex Pharmaceuticals Incorporated Inhibiteurs de la pyrazolopyridine kinase
WO2011094273A1 (fr) * 2010-01-27 2011-08-04 Vertex Pharmaceuticals Incorporated Inhibiteurs de la pyrazolopyridine kinase
WO2011094290A1 (fr) 2010-01-27 2011-08-04 Vertex Pharmaceuticals Incorporated Inhibiteurs des kinases à base de pyrazolopyrimidine
JP2013518113A (ja) 2010-01-27 2013-05-20 バーテックス ファーマシューティカルズ インコーポレイテッド ピラゾロピラジンキナーゼ阻害剤
MX2012013081A (es) 2010-05-12 2013-05-09 Vertex Pharma Compuestos utiles como inhibidores de cinasa atr.
WO2011143425A2 (fr) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Composés utilisables en tant qu'inhibiteurs de la kinase atr
JP6086326B2 (ja) 2010-05-24 2017-03-01 ユニヴァーシティー オブ ロチェスター 二環式ヘテロアリールキナーゼ阻害剤および使用方法
CA2816957A1 (fr) 2010-11-07 2012-05-10 Targegen, Inc. Compositions et procedes de traitement de la myelofibrose
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
TR201815685T4 (tr) 2011-04-01 2018-11-21 Genentech Inc Kanser tedavisi için akt ve mek inhibe edici bileşiklerin kombinasyonları.
CA2844699C (fr) 2011-04-01 2019-05-07 Genentech, Inc. Combinaisons de composes inhibiteurs d'akt et d'abiraterone et procedes d'utilisation
BR112014007721B1 (pt) 2011-09-30 2022-11-01 Vertex Pharmaceuticals Incorporated Processos para preparar compostos úteis como inibidores de atr quinase
MX2014003785A (es) 2011-09-30 2014-07-24 Vertex Phamaceuticals Inc Tratamiento del cancer de pancreas y del cancer de pulmon de celulas no pequeñas con inhibidores de atr.
TW201329025A (zh) 2011-11-01 2013-07-16 Astex Therapeutics Ltd 醫藥化合物
WO2013071067A1 (fr) * 2011-11-11 2013-05-16 Georgetown University Ligands nicotiniques substitués par un phényle, et leurs procédés d'utilisation
WO2013102145A1 (fr) 2011-12-28 2013-07-04 Global Blood Therapeutics, Inc. Composés d'aldéhydes hétéroaryles substitués et leurs procédés d'utilisation dans l'accroissement de l'oxygénation tissulaire
CA3142817A1 (fr) 2011-12-28 2013-07-04 Global Blood Therapeutics, Inc. Composes benzaldehyde substitues et procedes d'utilisation de ceux-ci dans l'augmentation de l'oxygenation des tissus
CA2869309C (fr) 2012-04-05 2021-02-09 Vertex Pharmaceuticals Incorporated Composes utiles comme inhibiteurs d'atr kinase et therapies combinees les utilisant
AU2013309868A1 (en) 2012-08-30 2015-03-12 Nippon Shinyaku Co., Ltd. Pyridine derivative and medicine
GB201216018D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Pharmacologically active compounds
GB201216017D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Inhibitor compounds
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
WO2014085795A1 (fr) 2012-11-30 2014-06-05 University Of Rochester Inhibiteurs de kinase de lignage mixte pour des thérapies pour le vih/sida
US9908867B2 (en) 2013-01-08 2018-03-06 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the Wnt signaling pathway and therapeutic uses thereof
AR094812A1 (es) * 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
JO3516B1 (ar) 2013-03-06 2020-07-05 Janssen Pharmaceutica Nv مُعدِّلات بنزإيميدازول-2-يل بيريميدين لمستقبل الهستامين h4
AU2014237340C1 (en) 2013-03-15 2018-11-08 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9604999B2 (en) 2013-03-15 2017-03-28 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
KR102293060B1 (ko) 2013-03-15 2021-08-23 글로벌 블러드 테라퓨틱스, 인크. 헤모글로빈 조정을 위한 화합물 및 이의 용도
US9422279B2 (en) 2013-03-15 2016-08-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US10266551B2 (en) 2013-03-15 2019-04-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US9458139B2 (en) 2013-03-15 2016-10-04 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US20140274961A1 (en) 2013-03-15 2014-09-18 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US8952171B2 (en) 2013-03-15 2015-02-10 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
US10100043B2 (en) 2013-03-15 2018-10-16 Global Blood Therapeutics, Inc. Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation
US9802900B2 (en) 2013-03-15 2017-10-31 Global Blood Therapeutics, Inc. Bicyclic heteroaryl compounds and uses thereof for the modulation of hemoglobin
SG11201507453VA (en) 2013-03-15 2015-10-29 Global Blood Therapeutics Inc Compounds and uses thereof for the modulation of hemoglobin
JP6463366B2 (ja) 2013-10-10 2019-01-30 イースタン バージニア メディカル スクール 12−リポキシゲナーゼ阻害物質としての4−((2−ヒドロキシ−3−メトキシベンジル)アミノ)ベンゼンスルホンアミド誘導体
CN105934425B (zh) 2013-11-15 2020-08-07 威斯塔解剖学和生物学研究所 Ebna1抑制剂和其使用方法
EA202092627A1 (ru) 2013-11-18 2021-09-30 Глобал Блад Терапьютикс, Инк. Соединения и их применения для модуляции гемоглобина
GB201402277D0 (en) 2014-02-10 2014-03-26 Sentinel Oncology Ltd Pharmaceutical compounds
JP6484640B2 (ja) 2014-02-14 2019-03-13 武田薬品工業株式会社 Gpr6のピラジンモジュレーター
GB201403536D0 (en) 2014-02-28 2014-04-16 Cancer Rec Tech Ltd Inhibitor compounds
PE20170127A1 (es) 2014-03-20 2017-03-30 Samumed Llc Indazol-3-carboxamidas 5-sustituidas y preparacion y uso de las mismas
BR112016022298B1 (pt) * 2014-04-02 2022-09-20 Bristol-Myers Squibb Company Inibidores de biarilcinase e composição que os compreende
MD20160112A2 (ro) 2014-04-25 2017-06-30 Pfizer Inc. Compuşi heteroaromatici şi utilizarea lor ca liganzi ai dopaminei D1
AR101198A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Pirimidinas 2,5-sustituidas como inhibidores de pde4b
AR101196A1 (es) 2014-07-16 2016-11-30 Gruenenthal Gmbh Compuestos de pirimidina sustituidos
RU2658821C1 (ru) 2014-08-18 2018-06-25 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Соль моноциклического производного пиридина и ее кристалл
WO2016040180A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine et ses utilisations thérapeutiques
WO2016040185A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 2-1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine et ses utilisations thérapeutiques
WO2016040190A1 (fr) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine et ses utilisations thérapeutiques
JP6746569B2 (ja) 2014-10-07 2020-08-26 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated 嚢胞性線維症膜貫通コンダクタンス制御因子のモジュレーターの共結晶
CN104370813A (zh) * 2014-10-22 2015-02-25 上海大学 异喹啉-6-甲醛的制备方法
CN104610229B (zh) * 2015-01-21 2017-01-18 上海皓元生物医药科技有限公司 一种是atp竞争性小分子akt抑制剂a443654的合成方法
MA41841A (fr) 2015-03-30 2018-02-06 Global Blood Therapeutics Inc Composés aldéhyde pour le traitement de la fibrose pulmonaire, de l'hypoxie, et de maladies auto-immunes et des tissus conjonctifs
BR112017024481B1 (pt) 2015-05-14 2020-11-17 The Wistar Institute Of Anatomy And Biology composto inibidor de ebna1, composição farmacêutica compreendendo dito composto e usos terapêuticos do mesmo
CN106265660B (zh) * 2015-05-21 2019-08-02 中国科学院合肥物质科学研究院 A674563在携带flt3突变型基因的急性白血病中的用途
SI3319959T1 (sl) 2015-07-06 2022-02-28 Alkermes, Inc. Hetero-halo inhibitorji histonske deacetilaze
US10421756B2 (en) 2015-07-06 2019-09-24 Rodin Therapeutics, Inc. Heterobicyclic N-aminophenyl-amides as inhibitors of histone deacetylase
US10226453B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017024015A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
WO2017023986A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles et leurs utilisations thérapeutiques
WO2017023988A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
WO2017023972A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
WO2017024003A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines et leurs utilisations thérapeutiques
WO2017023984A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines et leurs utilisations thérapeutiques
US10392383B2 (en) 2015-08-03 2019-08-27 Samumed, Llc 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023975A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines et leus utilisations thérapeutiques
US10463651B2 (en) 2015-08-03 2019-11-05 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof
US10166218B2 (en) 2015-08-03 2019-01-01 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017023980A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines et leurs utilisations thérapeutiques
WO2017024021A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles et leurs utilisations thérapeutiques
WO2017023987A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines et leurs utilisations thérapeutiques
US10519169B2 (en) 2015-08-03 2019-12-31 Samumed, Llc 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023996A1 (fr) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines et leurs utilisations thérapeutiques
US10206909B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
GB201514021D0 (en) 2015-08-07 2015-09-23 Arner Elias Set Jeno Novel Pyridines and their use in the treatment of cancer
US10688093B2 (en) 2015-09-09 2020-06-23 Lau Warren C Methods, compositions, and uses of novel Fyn kinase inhibitors
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
KR20180069005A (ko) 2015-10-26 2018-06-22 바이엘 크롭사이언스 악티엔게젤샤프트 농약으로서의 융합된 비사이클릭 헤테로사이클 유도체
CN108472290A (zh) 2015-11-06 2018-08-31 萨穆梅德有限公司 治疗骨关节炎
MX2018006832A (es) 2015-12-04 2018-11-09 Global Blood Therapeutics Inc Regimenes de dosificacion de 2-hidroxi-6-((2-(1-isopropil-1h-piraz ol-5-il)-piridin-3-il)-metoxi)-benzaldehido.
TWI752307B (zh) 2016-05-12 2022-01-11 美商全球血液治療公司 新穎化合物及製造化合物之方法
PT3464285T (pt) 2016-06-01 2022-12-20 Biosplice Therapeutics Inc Processo para preparar n-(5-(3-(7-(3-fluorofenil)-3himidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida
JP6946412B2 (ja) 2016-07-18 2021-10-06 ヤンセン ファーマシューティカ エヌ.ベー. タウpet画像化リガンド
TW202332423A (zh) 2016-10-12 2023-08-16 美商全球血液治療公司 包含2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)吡啶-3-基)甲氧基)-苯甲醛之片劑
AU2017345699A1 (en) 2016-10-21 2019-05-16 Samumed, Llc Methods of using indazole-3-carboxamides and their use as Wnt/B-catenin signaling pathway inhibitors
WO2018085865A1 (fr) 2016-11-07 2018-05-11 Samumed, Llc Formulations injectables à dose unique prêtes à l'emploi
EP3541431B1 (fr) * 2016-11-16 2024-04-17 The General Hospital Corporation Agents d'imagerie de myéloperoxydase
MD3570834T2 (ro) 2017-01-11 2022-04-30 Alkermes Inc Inhibitori biciclici ai histon deacetilazei
MX2019009356A (es) 2017-02-07 2019-09-19 Oblique Therapeutics Ab Sulfinilpiridinas y su uso en el tratamiento del cancer.
WO2018146469A1 (fr) 2017-02-07 2018-08-16 Oblique Therapeutics Ab Pyridines à substitution hétéroarylsulfonyle et leur utilisation dans le traitement du cancer
MA47458A (fr) 2017-02-07 2019-12-18 Oblique Therapeutics Ab Pyridines à substitution hydrocarbylsulfonyle et leur utilisation dans le traitement du cancer
JP2020506244A (ja) 2017-02-07 2020-02-27 オブリーク セラピューティクス アーベー ヘテロシクリルスルホニル置換ピリジンおよび癌の治療におけるそれらの使用
GB201709840D0 (en) 2017-06-20 2017-08-02 Inst Of Cancer Research: Royal Cancer Hospital Methods and medical uses
MA49839B1 (fr) 2017-08-07 2022-05-31 Alkermes Inc Inhibiteurs bicycliques de la histone déacétylase
MX2020008610A (es) 2018-03-28 2020-09-21 Eisai R&D Man Co Ltd Agente terapeutico para carcinoma hepatocelular.
CN112543634A (zh) 2018-05-17 2021-03-23 威斯达研究所 Ebna1抑制剂晶体形式及其制备和使用方法
CN113227103A (zh) 2018-09-18 2021-08-06 尼坎医疗公司 作为src同源-2磷酸酶抑制剂的三取代的杂芳基衍生物
ES2966707T3 (es) 2018-10-01 2024-04-23 Global Blood Therapeutics Inc Moduladores de la hemoglobina para el tratamiento de la drepanocitosis
WO2022058344A1 (fr) 2020-09-18 2022-03-24 Bayer Aktiengesellschaft Pyrido[2,3-d]pyrimidin-4-amines en tant qu'inhibiteurs de sos1
EP4074317A1 (fr) 2021-04-14 2022-10-19 Bayer AG Dérivés de phosphore en tant que nouveaux inhibiteurs de sos1
EP4173674A1 (fr) * 2021-10-26 2023-05-03 Perha Pharmaceuticals Dérivés d'imidazolone en tant qu'inhibiteurs de kinases de protéine en particulier, dyrk1a, clk1 et/ou clk4
CN115353508B (zh) * 2022-08-24 2023-07-21 中国药科大学 5-吡啶-1h-吲唑类化合物、药物组合物和应用
CN115417816B (zh) * 2022-09-05 2024-01-26 江苏南大光电材料股份有限公司 一种3,6-二溴-1-氯-异喹啉的制备方法
WO2024056782A1 (fr) 2022-09-16 2024-03-21 Bayer Aktiengesellschaft Dérivés de pyrido[3,4-d]pyrimidine substitués par sulfone pour le traitement du cancer
WO2024079252A1 (fr) 2022-10-13 2024-04-18 Bayer Aktiengesellschaft Inhibiteurs de sos1

Citations (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4179563A (en) * 1978-05-19 1979-12-18 Warner-Lambert Company 3-Aryloxy-substituted-aminopyridines and methods for their production
WO1993010114A1 (fr) * 1991-11-20 1993-05-27 Smithkline Beecham Plc Derives du 3-pyridinol et leur utilisation comme medicaments
US5629325A (en) * 1996-06-06 1997-05-13 Abbott Laboratories 3-pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission
WO1999031088A1 (fr) * 1997-12-12 1999-06-24 Abbott Laboratories Inhibiteurs d'angiogenese a base de triazine
WO1999058523A1 (fr) * 1998-05-14 1999-11-18 G.D. Searle & Co. PYRAZOLES A SUBSTITUTION 1,5-DIARYLE COMME INHIBITEURS DE LA PROTEINE p38 KINASE
WO1999061406A2 (fr) * 1998-05-22 1999-12-02 Abbott Laboratories Medicament anti-angiogenique pour le traitement du cancer, de l'arthrite et de la retinopathie
US6030969A (en) * 1998-04-09 2000-02-29 Abbott Laboratories 5,6,7-trisubstituted-4-aminopyrido[2,3-D] pyrimidine compounds
WO2000010997A1 (fr) * 1998-08-25 2000-03-02 Ortho-Mcneil Pharmaceutical, Inc. Pyridyl ethers et thioethers tenant lieu de ligands pour le recepteur de l'acetycholine nicotinique, et application therapeutique
WO2000023444A1 (fr) * 1998-10-21 2000-04-27 Abbott Laboratories Composes de 4-aminopyrido[2,3-d]pyrimidine a disubstitution 5,7
WO2000073264A1 (fr) * 1999-05-28 2000-12-07 Abbott Laboratories Inhibiteurs de proliferation cellulaire
WO2001019817A2 (fr) * 1999-09-14 2001-03-22 Abbott Laboratories Composes d'ether 3-pyrrolidinyloxy-3'-pyridyle utilises comme regulateurs de la transmission synaptique chimique
WO2001019829A2 (fr) * 1999-09-17 2001-03-22 Basf Aktiengesellschaft Pyrazolopyrimidines en tant qu'agents therapeutiques
WO2001057018A1 (fr) * 2000-02-02 2001-08-09 Abbott Laboratories Inhibiteurs d'azaazulene de la p38 map kinase ou du tnf-alpha
WO2001057040A1 (fr) * 2000-02-03 2001-08-09 Abbott Laboratories Composes de 4-aminopyrido[2,3-d]pyrimidine a disubstitution en position 6,7
WO2001070687A1 (fr) * 2000-03-23 2001-09-27 Bayer Aktiengesellschaft Indoles pour le traitement de maladies pouvant etre traitees a l'aide d'hormones thyroidiennes
WO2001081316A2 (fr) * 2000-04-27 2001-11-01 Abbott Laboratories Inhibiteurs de phenyle farnesyltransferase substitues
WO2002010137A2 (fr) * 2000-07-31 2002-02-07 Signal Pharmaceuticals, Inc. Derives d'indazole utilises comme inhibiteurs de jnk et compositions et methodes associees a ceux-ci
WO2002022601A1 (fr) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Composes pyrazoliques utiles comme inhibiteurs de la proteine kinase
WO2002050065A2 (fr) * 2000-12-21 2002-06-27 Vertex Pharmaceuticals Incorporated Composes de pyrazole presentant une grande utilite comme inhibiteurs de proteine kinase

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9326136D0 (en) 1993-12-22 1994-02-23 Erba Carlo Spa Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents
GB9401460D0 (en) 1994-01-26 1994-03-23 Rhone Poulenc Rorer Ltd Compositions of matter
US5593994A (en) 1994-09-29 1997-01-14 The Dupont Merck Pharmaceutical Company Prostaglandin synthase inhibitors
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US6147106A (en) 1997-08-20 2000-11-14 Sugen, Inc. Indolinone combinatorial libraries and related products and methods for the treatment of disease
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
GB9611797D0 (en) 1996-06-06 1996-08-07 Pharmacia Spa Substituted quinolylmethylen-oxindole analogues as tyrosine kinase inhibitors
WO1998002434A1 (fr) 1996-07-13 1998-01-22 Glaxo Group Limited Composes heterocycliques condenses en tant qu'inhibiteurs de la proteine tyrosine kinase
US5935977A (en) 1996-09-25 1999-08-10 Ss Pharmaceutical Co., Ltd. Substituted vinyl pyridine derivative and drugs containing the same
CO4940469A1 (es) 1997-03-05 2000-07-24 Sugen Inc Composicion oral de estabilidad mejorada que comprende un derivado de indolinona y una mezcla de gliceridos o esteres de polietilenglicol
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
CN1250526C (zh) 1998-05-29 2006-04-12 苏根公司 吡咯取代的2-吲哚满酮蛋白激酶抑制剂
WO1999065875A1 (fr) 1998-06-17 1999-12-23 Geron Corporation Inhibiteurs de la telomerase
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
EP1117397A1 (fr) 1998-08-31 2001-07-25 Sugen, Inc. Derives de 2-indolinone a geometrie limitee utilises en tant que modulateurs de l'activite de la proteine kinase
JP2002525356A (ja) 1998-09-25 2002-08-13 ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト 新規置換インドリノン、それらの調製及び薬物としてのそれらの使用
US6462036B1 (en) * 1998-11-06 2002-10-08 Basf Aktiengesellschaft Tricyclic pyrazole derivatives
BR9916735A (pt) 1998-12-31 2001-09-25 Sugen Inc Compostos de 3-heteroarilidenil-2-indolinona para a modulação da atividade das cinases protéicas e para uso na quimioterapia do cancêr
AUPP873799A0 (en) 1999-02-17 1999-03-11 Fujisawa Pharmaceutical Co., Ltd. Pyridine compounds
EP1165513A1 (fr) 1999-03-24 2002-01-02 Sugen, Inc. Composes d'indolinone tels que des inhibiteurs de kinase
ATE316527T1 (de) 1999-08-27 2006-02-15 Boehringer Ingelheim Pharma Substituierte indolinone als tyrosinkinase inhibitoren
DE19949209A1 (de) 1999-10-13 2001-04-19 Boehringer Ingelheim Pharma In 5-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
UA75054C2 (uk) 1999-10-13 2006-03-15 Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу
JP2003512396A (ja) 1999-10-26 2003-04-02 ザ・ユニバーシティ・オブ・テキサス・サウスウエスタン・メディカル・センター インドリン化合物を投与することを含む脱毛症の処置方法
WO2001049287A1 (fr) 1999-12-30 2001-07-12 Sugen, Inc. Composes 3-heteroarylidenyl-2-indolinone destines a moduler l'activite des proteines kinases et a etre utilises en chimiotherapie du cancer
JP2003520855A (ja) 2000-01-28 2003-07-08 アストラゼネカ アクチボラグ 化学的化合物
WO2001060814A2 (fr) 2000-02-15 2001-08-23 Sugen, Inc. Inhibiteurs de la proteine kinase 2-indolinone a substitution pyrrole
AU3704101A (en) 2000-02-17 2001-08-27 Amgen Inc Kinase inhibitors
EP1259236A4 (fr) 2000-02-25 2004-11-03 Merck & Co Inc Inhibiteurs de tyrosine-kinase
US6420382B2 (en) 2000-02-25 2002-07-16 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1265992A2 (fr) 2000-03-08 2002-12-18 Zealand Pharma A/S SUBSTANCES ET PROCEDES LIES A LA DEGRADATION DE Cdc25A EN REPONSE A UN DOMMAGE DE L'ADN
MY128450A (en) 2000-05-24 2007-02-28 Upjohn Co 1-(pyrrolidin-1-ylmethyl)-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
EP1294688A2 (fr) 2000-06-02 2003-03-26 Sugen, Inc. Derives d'indolinone comme inhibiteurs de phosphatase/proteine kinase

Patent Citations (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4179563A (en) * 1978-05-19 1979-12-18 Warner-Lambert Company 3-Aryloxy-substituted-aminopyridines and methods for their production
WO1993010114A1 (fr) * 1991-11-20 1993-05-27 Smithkline Beecham Plc Derives du 3-pyridinol et leur utilisation comme medicaments
US5629325A (en) * 1996-06-06 1997-05-13 Abbott Laboratories 3-pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission
US6127386A (en) * 1996-06-06 2000-10-03 Abbott Laboratories 3-Pyridyloxymethyl heterocyclic ether compounds useful in controlling chemical synaptic transmission
WO1999031088A1 (fr) * 1997-12-12 1999-06-24 Abbott Laboratories Inhibiteurs d'angiogenese a base de triazine
US6030969A (en) * 1998-04-09 2000-02-29 Abbott Laboratories 5,6,7-trisubstituted-4-aminopyrido[2,3-D] pyrimidine compounds
WO1999058523A1 (fr) * 1998-05-14 1999-11-18 G.D. Searle & Co. PYRAZOLES A SUBSTITUTION 1,5-DIARYLE COMME INHIBITEURS DE LA PROTEINE p38 KINASE
WO1999061406A2 (fr) * 1998-05-22 1999-12-02 Abbott Laboratories Medicament anti-angiogenique pour le traitement du cancer, de l'arthrite et de la retinopathie
WO2000010997A1 (fr) * 1998-08-25 2000-03-02 Ortho-Mcneil Pharmaceutical, Inc. Pyridyl ethers et thioethers tenant lieu de ligands pour le recepteur de l'acetycholine nicotinique, et application therapeutique
WO2000023444A1 (fr) * 1998-10-21 2000-04-27 Abbott Laboratories Composes de 4-aminopyrido[2,3-d]pyrimidine a disubstitution 5,7
WO2000073264A1 (fr) * 1999-05-28 2000-12-07 Abbott Laboratories Inhibiteurs de proliferation cellulaire
WO2001019817A2 (fr) * 1999-09-14 2001-03-22 Abbott Laboratories Composes d'ether 3-pyrrolidinyloxy-3'-pyridyle utilises comme regulateurs de la transmission synaptique chimique
WO2001019829A2 (fr) * 1999-09-17 2001-03-22 Basf Aktiengesellschaft Pyrazolopyrimidines en tant qu'agents therapeutiques
WO2001057018A1 (fr) * 2000-02-02 2001-08-09 Abbott Laboratories Inhibiteurs d'azaazulene de la p38 map kinase ou du tnf-alpha
WO2001057040A1 (fr) * 2000-02-03 2001-08-09 Abbott Laboratories Composes de 4-aminopyrido[2,3-d]pyrimidine a disubstitution en position 6,7
WO2001070687A1 (fr) * 2000-03-23 2001-09-27 Bayer Aktiengesellschaft Indoles pour le traitement de maladies pouvant etre traitees a l'aide d'hormones thyroidiennes
WO2001081316A2 (fr) * 2000-04-27 2001-11-01 Abbott Laboratories Inhibiteurs de phenyle farnesyltransferase substitues
WO2002010137A2 (fr) * 2000-07-31 2002-02-07 Signal Pharmaceuticals, Inc. Derives d'indazole utilises comme inhibiteurs de jnk et compositions et methodes associees a ceux-ci
WO2002022601A1 (fr) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Composes pyrazoliques utiles comme inhibiteurs de la proteine kinase
WO2002050065A2 (fr) * 2000-12-21 2002-06-27 Vertex Pharmaceuticals Incorporated Composes de pyrazole presentant une grande utilite comme inhibiteurs de proteine kinase

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (1998), 8(19), 2797-2802 *
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2000), 10(10), 1063-1066 *
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2001), 11(5), 631-633 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; HOLLADAY, MARK W. ET AL: "Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice", XP002240028, retrieved from STN Database accession no. 130:75736 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; LEE, JUNG ET AL: "Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor", XP002240027, retrieved from STN Database accession no. 133:171774 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; LIN, N.-H. ET AL: "Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic receptor ligand", XP002240026, retrieved from STN Database accession no. 135:19528 *

Cited By (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9365548B2 (en) 2006-03-31 2016-06-14 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor
US9381192B2 (en) 2009-08-10 2016-07-05 Samumed, Llc Indazole inhibitors of the Wnt signal pathway and therapeutic uses thereof
US9446035B2 (en) 2009-12-21 2016-09-20 Samumed, Llc 1H-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
US8901150B2 (en) 2009-12-21 2014-12-02 Samumed, Llc 1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
US8846714B2 (en) 2009-12-21 2014-09-30 Samumed, Llc 1H-pyrazolo[3,4-β]pyridines and therapeutic uses thereof
US9221793B2 (en) 2011-09-14 2015-12-29 Samumed, Llc Indazole-3-carboxamides and their use as Wnt/β-catenin signaling pathway inhibitors
US8987298B2 (en) 2012-04-04 2015-03-24 Samumed, Llc Indazole inhibitors of the Wnt signal pathway and therapeutic uses thereof
US9199991B2 (en) 2012-04-04 2015-12-01 Samumed, Llc Indazole inhibitors of the WNT signal pathway and therapeutic uses thereof
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
US9012472B2 (en) 2012-05-04 2015-04-21 Samumed, Llc 1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
US9233104B2 (en) 2012-05-04 2016-01-12 Samumed, Llc 1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
US8883822B2 (en) 2012-05-04 2014-11-11 Samumed, Llc 1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
US9586977B2 (en) 2012-05-04 2017-03-07 Samumed, Llc 1H-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
US9394285B2 (en) 2013-03-15 2016-07-19 Pfizer Inc. Indole and indazole compounds that activate AMPK
US9447071B2 (en) 2014-02-07 2016-09-20 Global Blood Therapeutics, Inc. Crystalline polymorphs of the free base of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
US9475825B2 (en) 2014-09-08 2016-10-25 Samumed, Llc 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridine and therapeutic uses thereof
US9475807B2 (en) 2014-09-08 2016-10-25 Samumed, Llc 2-(1H-indazol-3-yl)-1H-imidazo[4,5-C]pyridine and therapeutic uses thereof
US9493487B2 (en) 2014-09-08 2016-11-15 Samumed, Llc 3-(1H-imidazo[4,5-C]pyridin-2-YL)-1H-pyrazolo[3,4-B]pyridine and therapeutic uses thereof
US9540398B2 (en) 2014-09-08 2017-01-10 Samumed, Llc 3-(1h-imidazo[4,5-C]pyridin-2-yl)-1h-pyrazolo[3,4-C]pyridine and therapeutic uses thereof
US9546185B2 (en) 2014-09-08 2017-01-17 Samumed, Llc 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridine and therapeutic uses thereof

Also Published As

Publication number Publication date
US6831175B2 (en) 2004-12-14
US20030199511A1 (en) 2003-10-23
WO2003051366A2 (fr) 2003-06-26
US20030187026A1 (en) 2003-10-02

Similar Documents

Publication Publication Date Title
WO2003051366A3 (fr) Inhibiteurs de kinase
WO2006050109A3 (fr) Nouveaux inhibiteurs de kinase
WO2007079164A3 (fr) Inhibiteurs de protéines kinases
IL171976A0 (en) Indazole, benzisoxazole, and banzisothiazole kinase inhibitors
WO2004058769A3 (fr) Compositions utiles en tant qu'inhibiteurs des proteine kinases
WO2002096905A8 (fr) Composes de thiazole inhibiteurs des proteines kinases
PL1635835T3 (pl) Pochodne 2-aminopirymidyny jako inhibitory kinazy RAF
WO2006070195A8 (fr) Composes de pyrazole regulant l’activite de kinases cdk, gsk et aurora
MXPA03010961A (es) Compuestos de tiazol utiles como inhibidores de proteinas cinasas.
AU2003297160A1 (en) Benzisoxazole derivatives useful as inhibitors of protein kinases
WO2006047503A3 (fr) Inhibiteurs de la c-fms kinase
HK1106247A1 (en) 3-(indazol-5-yl)-(1,2,4)triazine derivatives and related compounds as protein kinase inhibitors for the treatment of cancer
MXPA02005844A (es) Inhibidores de cinasas de proteina.
WO2002096361A3 (fr) Derives de 5-aralkylsulfonyl-3-(pyrrol-2-ylmethylidene)-2-indolinone utilises comme inhibiteurs de kinase
WO2008017361A3 (fr) Dérivés de 2-(hétérocyclylbenzyl)-pyridazinone
IL173348A0 (en) Thienopyridine and furopyridine kinase inhibitors
WO2004031401A3 (fr) Nouveaux inhibiteurs de tyrosine kinases
WO2006004636A3 (fr) Inhibiteurs de kinase heterocycliques accoles
WO2001060814A3 (fr) Inhibiteurs de la proteine kinase 2-indolinone a substitution pyrrole
CA2400447A1 (fr) Inhibiteurs de kinases
WO2006047479A3 (fr) Inhibiteurs de c-fms kinase
WO2003076398A3 (fr) Inhibiteurs de kinases
WO2000043373A3 (fr) Inhibiteurs de kinase
WO2004063151A3 (fr) Nouveaux inhibiteurs de tyrosine kinase
MXPA05009151A (es) Inhibidores de cinasa heterociclica.

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SC SD SE SG SK SL TJ TM TN TR TT TZ UA UG UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR IE IT LU MC NL PT SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: PA/a/2004/005810

Country of ref document: MX

Ref document number: 2003552299

Country of ref document: JP

Ref document number: 2470214

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 2002790126

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 2002790126

Country of ref document: EP